SH-4-54 - STAT 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESH-4-54Cat. No.: HY-16975CAS No.: 1456632-40-8分式: CHFNOS分量: 610.59作靶点: STAT作通路: JAK/STAT Signaling; Stem Cell/Wnt储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (163.78 mM; Need u

2、ltrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.09 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.09 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 SH-4-54是STAT 的抑制剂，与 STAT3 和 STAT5 结合的 KDs 值分别为300，

3、464 nM。IC50 & Target STAT3 STAT5300 nM (Kd) 464 nM (Kd)体外研究 SH-4-54 potently kills glioblastoma brain cancer stem cells (BTSCs) and effectively suppresses STAT3phosphorylation and its downstream transcriptional targets at low nM concentrations.SH-4-54 showsunprecedented cytotoxicity in human BTSCs,

4、displays no toxicity in human fetal astrocytes, potentlysuppresses pSTAT3 with nanomolar IC50s, inhibiting STAT3s downstream targets, and shows nodiscernible off-target effects at therapeutic doses 1.体内研究 SH-4-54 exhibits blood-brain barrier permeability potently controls glioma tumor growth, and in

5、hibits pSTAT3in vivo. SH-4-54 demonstrates the power of STAT3 inhibitors for the treatment of BTSCs and validates thetherapeutic efficacy of a STAT3 inhibitor for GBM clinical application.SH-4-54 decreases pSTAT3 expressionin tumor cells of treated mice. SH-4-54 appears to decrease proliferation and

6、 increase apoptosis of treatedtumors 1.户使本产品发表的科研献 Biochem Biophys Res Commun. 2017 Mar 4;484(2):311-317.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Haftchenary S, et al. Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma.ACS Med Chem Lett. 2013 Sep 8;4(11):1102-1107.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: